The present invention relates to novel pharmacologically acceptable salts of 5-aminosalicylic acid O-sulfate, processes for the preparation thereof and drugs containing same which are suitable for the treatment of colitis ulcerosa, enteritis regionalis Crohn (morbus Crohn), chronic nonspecific colitis and diverticulitis.
The standard preparation for the treatment of said diseases has so far been salazosulfapyridine. Said compound has mostly been orally administered and is probably bacterially decomposed in the colon to give the two metabolites 5-aminosalicylic acid and sulfapyridine. The metabolite 5-aminosalicylic acid has appeared to be the active component while the frequently observed side-effects are to be attributed to the metabolite sulfapyridine; cf. Khan et al., Lancet 2, 892 (1977). As 5-aminosalicylic acid is instable and virtually cannot be conveyed into the colon via the oral route, there has already been contemplated by Khan, loc. cit., the possibility of synthesizing a new substance which does not exhibit said drawbacks inherent to the known salazosulfaypyridine.
From German Offenlegungsschrift (Published Unexamined Patent Application) No. 30 27 013 by applicants there has been known an agent for treating colitis ulcerosa, enteritis regionalis Crohn (morbus Crohn), chronic nonspecific colitis and diverticulitis, which agent contains salicylic azobenzoic acid. Said agent is being successfully tested under clinical conditions. However, the salicylic azobenzoic acid contains an azo moiety which is rated to be toxicologically doubtful and, hence, should be avoided in drugs if possible.